Discovery of Biaryl Amides as Potent, Orally Bioavailable, and CNS Penetrant RORγt Inhibitors

[Image: see text] A novel series of biaryl amides was identified as RORγt inhibitors through core replacement of a starting hit 1. Structure–activity relationship exploration on the biaryl moiety led to discovery of potent RORγt inhibitors with good oral bioavailability and CNS penetration. Compound...

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Detalles Bibliográficos
Publicado en:ACS Med Chem Lett
Main Authors: Wang, Yonghui, Cai, Wei, Cheng, Yaobang, Yang, Ting, Liu, Qian, Zhang, Guifeng, Meng, Qinghua, Han, Fangbin, Huang, Yafei, Zhou, Ling, Xiang, Zhijun, Zhao, Yong-Gang, Xu, Yan, Cheng, Ziqiang, Lu, Sijie, Wu, Qianqian, Xiang, Jia-Ning, Elliott, John D., Leung, Stewart, Ren, Feng, Lin, Xichen
Formato: Artigo
Idioma:Inglês
Publicado: American Chemical Society 2015
Acceso en liña:https://ncbi.nlm.nih.gov/pmc/articles/PMC4499822/
https://ncbi.nlm.nih.gov/pubmed/26191367
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.5b00122
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